Luliberin analogues containing the nuclear localization sequence of the SV-40 virus T-antigen

作者：Burov S V^*; Yablokova T V; Dorosh M Yu; Krivizyuk E V; Efremov A M; Orlov S V

来源：Russian Journal of Bioorganic Chemistry, 2010, 36(5): 581-588.

DOI：10.1134/S1068162010050055

• anticancer activity
• luliberin
• nuclear localization signal
• palmitic acid

With the goal of improving the efficacy of anticancer drugs due to the directed delivery to intracellular targets, a set of luliberin analogues containing the nuclear localization signal (NLS) of the SV-40 virus large T-antigen has been synthesized. The NLS was attached to the parent molecule via the D-lysine E >-amino group introduced into position 1 or 6 of the peptide sequence using the orthogonal protection strategy. Biological tests demonstrated that this modification supported in vitro a significant increase in the cytotoxic activity of luliberin analogues containing palmitoyl residues. The influence of the studied peptides on tumor cells was not associated with the distortion of the membrane integrity, which was confirmed by experiments with normal fibroblasts used as a control.

• 出版日期2010-9